Transglutaminase inhibitors and methods of use thereof

Abstract

Transglutaminase inhibitors and methods of use thereof are provided.

What is claimed is: 
     
       1. A pharmaceutical formulation comprising:
 an effective dose of a tTGase inhibitor, wherein said tTGase inhibitory moiety is: 
 
       
         
           
           
               
               
           
         
         wherein R 1  is quinolin-3-ylmethyl ester and R 2  is selected from the group consisting of 5-fluoro-1H-indol-3-yl, (S)-Bn, (S)—CO 2 Me, (S)-Me, (R)-Bn, (S)—CH 2 CONHBn, (S)-(1H-inol-yl)-methyl, (S)-(4-hydroxy-phenyl)-methyl, OMe, OtBu, Gly, Gly-NH 2 , LPY, LPF—NH 2 ; 
         R 3  is selected from Cl, and Br; n is 0; and X is selected from the group consisting of O and NH. 
       
     
     
       2. The formulation of  claim 1 , wherein R 2  is 5-fluoro-1H-indol-3-yl.